Molecular Glues for Targeted Protein Degradation: From Serendipity to Rational Discovery,Journal of Medicinal Chemistry

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Molecular Glues for Targeted Protein Degradation: From Serendipity to Rational Discovery
Journal of Medicinal Chemistry ( IF 6.8 ) Pub Date : 2021-07-28 , DOI: 10.1021/acs.jmedchem.1c00895
Guoqiang Dong ₁ , Yu Ding ₂ , Shipeng He ₃ , Chunquan Sheng ₁

Affiliation

Targeted protein degradation is a promising area in the discovery and development of innovative therapeutics. Molecular glues mediate proximity-induced protein degradation and have intrinsic advantages over heterobifunctional proteolysis-targeting chimeras, including unprecedented mechanisms, distinct biological activities, and favorable physicochemical properties. Classical molecular glue degraders have been identified serendipitously, but rational discovery and design strategies are emerging rapidly. In this review, we aim to highlight the recent advances in molecular glues for targeted protein degradation and discuss the challenges in developing molecular glues into therapeutic agents. In particular, discovery strategies, action mechanisms, and representative case studies will be addressed.

中文翻译：

用于靶向蛋白质降解的分子胶：从偶然发现到理性发现

靶向蛋白质降解是发现和开发创新疗法的一个有前途的领域。分子胶介导邻近诱导的蛋白质降解，并且具有优于异双功能蛋白水解靶向嵌合体的内在优势，包括前所未有的机制、独特的生物活性和有利的物理化学特性。经典的分子胶降解剂已被偶然发现，但合理的发现和设计策略正在迅速出现。在这篇综述中，我们旨在强调用于靶向蛋白质降解的分子胶的最新进展，并讨论将分子胶开发成治疗剂的挑战。特别是，将讨论发现策略、行动机制和代表性案例研究。

更新日期：2021-08-12

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